Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P61278 (somatostatin)
 22,083 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Somatostatin-receptor scintigraphy has been in clinical use for several years. Most of the experience with somatostatin tumor scintigraphy has been obtained with gastro-enteropathic (GEP) tumors and carcinoids. Clinical applications of somatostatin imaging have been reported in small-cell lung carcinomas, malignant lymphomas, renal-cell carcinomas, breast cancers and medullary thyroid cancers. Somatostatin analogues were initially applicable in larger medical institutions because of the necessity for radioactive labeling with iodine (octreotide to [123I-Tyr3]-octreotide); however, the clinical results with iodinated analogues were worse than the relatively new analogue [111In-DTPA-D-Phe1]octreotide, now available as Octreoscan. This review describes the current status of the clinical application of somatostatin receptor imaging, together with our own experience in carcinoids, GEP tumors and medullary thyroid carcinomas.
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PMID:[Somatostatin receptor scintigraphy. Methodology, indications, results]. 882 Mar 76

Somatostatin analogue scintigraphy represents a new technique employing radiolabelled peptides to detect specific receptor-bearing lesions. 111Indium diethylene-triaminopentaacetic acid-linked octreotide (111In-DTPA-D-Phe1-octreotide), also known as [111In]pentetreotide or OctreoScan, is now established in the management of patients with neueroendocrine gastrointestinal tract and pancreatic tumours, and has proved effective in localizing disease sites in lung, breast and medullary thyroid carcinomas, lymphomas, meningiomas and others. In these conditions (a) the imaging of all disease sites at a single sitting (in a proportion of patients) thereby making further investigations unnecessary, (b) the localization of otherwise unexpected metastatic deposits and (c) the detection of residual disease not found by other means suggest that [111In]pentetreotide may be a useful adjunct in the diagnostic evaluation of patients with somatostatin receptor-bearing tumours.
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PMID:Radiolabelled somatostatin analogue scintigraphy in oncology. 882 83

The purpose of this prospective study was to compare the ability of radiolabelled somatostatin analogue (RSA) and metaiodobenzylguanidine (MIBG) scintigraphy to display carcinoid tumours. Forty patients were studied after radiological assessment based on clinical symptomatology. These patients had radiologically demonstrated tumours (n=28), resected tumours discovered to be of the carcinoid type (n=5) or clinically and biologically suspected carcinoid tumours (n=7). They underwent indium-111 DTPA-pentetreotide or iodine-123-Tyr-3-octreotide and 131I-MIBG scintigraphy. The results were compared with those of complementary surgical or morphological examinations and analysed according to the site of the tumour and the symptomatology. In the case of 31 patients with a total of 55 tumoral sites, the sensitivity of the initial radiological assessment, of RSA and of MIBG was 96%, 86% and 64%, respectively, for the detection of at least one tumour per patient, but 51%, 85% and 51%, respectively, for the total number of sites. No site was detected solely by MIBG. The concordance between RSA and MIBG was better when all sites were considered (kappa index+0.44) than for only extrahepatic abdominal tumoral sites (kappa index+0.095). Abdominal, thoracic or bone marrow tumours were more easily detected with RSA than with MIBG. Hepatic invasion (21 cases) was more easily detected by radiology (sensitivity 100%) than by RSA and MIBG, both of which displayed a sensitivity of 80%, but with differences in uptake intensity. Tumour detection using MIBG was more significantly linked with flush (P<0.01) than with diarrhoea (P>0.10). In the assessment of carcinoid tumours, RSA scintigraphy should be carried out initially (just after hepatic ultrasonography) and supplemented by MIBG, as comparison of the studies serves to guide therapeutic options and might be valuable for prognosis.
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PMID:Comparison of somatostatin analogue and metaiodobenzylguanidine scintigraphy for the detection of carcinoid tumours. 885 40

Sandostatin, a synthetic octapeptide analog of a native hormone somatostatin, was labeled with a commonly available, inexpensive radionuclide, 99mTc, and evaluated for its suitability for in vivo imaging. Labeling was accomplished by reduction of the cystine bridge, which provided two sulfhydryl groups for chelation with 99mTc. The complex was examined for thermodynamic stability in vitro and in experimental animals. Receptor specificity of the complex was determined using rat brain cortex membrane rich in somatostatin receptors, and its tissue distribution was studied in nude mice bearing human prostate cancer. In these studies, 99mTc-labeled oxytocin, a nonspecific peptide with similar molecular weight, served as a control and 111In-DTPA-octreotide served as a standard. The labeling method was simple, did not require protecting and deprotecting functional groups and yields were high (ca. 70%). The in vitro and in vivo stability was excellent, and Kd values were in the nanomolar range, similar to those of 111In-DTPA-octreotide. At 24 hours post-injection, the tumor uptake for 99mTc-Sandostatin, expressed as percent of injected dose per gram (% ID/g), was higher, but the tumor/blood and tumor/muscle ratios were lower than those for 111In-DTPA-octreotide. This agent, with its improved target-to-nontarget ratios, should prove to be of value for imaging somatostatin receptor-positive tumors.
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PMID:Sandostatin labeled with 99mTc: in vitro stability, in vivo validity and comparison with 111In-DTPA-octreotide. 887 94

We examined the potential of radiolabeled somatostatin analogs, 125I-Tyr-3-octreotide (125I-octreotide), (111)In-DTPA(diethylenetriaminepentaacetatic acid)-D-Phe-1-octreotide (111In-octreotide), and 188Re-octreotide for targeting small-cell lung cancer (SCLC) in a mouse model. Tyr-3-octreotide was labeled with 125I by the chloramine T method, and (111)In-octreotide was obtained as a kit, while 188Re was eluted from a 188W/188Re generator, and octreotide was directly labeled with 188Re by reducing disulfide bonds. The 125I-, 111In-, and 188Re-octreotides were injected i.v. into athymic mice bearing NCI-H69 tumors, and the biodistributions were determined at 15 min, and 2, 4, 8, and 24 h. Tumor uptakes were 0.5+/-0.2, 0.3+/-0.1, 0.3+/-0.1 %ID/g, and tumor-to-blood ratios were 1.8, 11.9, 1.2 at 8 h for 125I-, 111In-, and 188Re-octreotides, respectively. Accumulations of 111In-octreotide in normal tissues were lower than those of 125I- and 188Re-octreotides. 188Re-octreotide can be used to localize SCLC lesions as efficiently as radioiodinated octreotide. However, 111In-octreotide was the most suitable agent to obtain high tumor-to-normal tissue contrast for localizing SCLC.
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PMID:Localization of small-cell lung cancer xenografts with iodine-125-, indium-111-, and rhenium-188-somatostatin analogs. 887 64

The peptide somatostatin and its analog octreotide play an important role in neoplasia where their actions have been shown to be mediated by specific somatostatin receptors located in the tumor tissue. The identification of a high density of SS receptors in vitro in different types of human tumors has provided completely new and attractive possibilities for their diagnostic localization in vivo. This can be achieved by intravenous injection of 123I-[Tyr3]-octreotide or 111In-DTPA-D-Phe1-octreotide in patients suspected of having SS receptor-positive tumors and by subsequent localization of the tumors with gamma camera scintigraphy techniques. Hot spots representing radioligand binding on SS receptor-positive tumors are visualized with this method. This new SS receptor imaging method may help the clinicians for the localization of the primary tumor and its metastases, for the staging of certain tumors, to predict a successful SS therapy, and as a prognostic or differential diagnostic marker. It may also be of use in non-tumoral pathologies, to localize selected inflammatory processes and to monitor anti-inflammatory therapy. Somatostatin receptor imaging represents the first example of the clinical use of a small peptide as an efficient in vivo diagnostic tool and may be considered as a paradigm for further research on the role and the potential diagnostic use of other peptide receptors in pathological states.
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PMID:Receptor imaging of human diseases using radiolabeled peptides. 890 52

We have studied prospectively 47 patients with CNS tumours including 16 meningiomas and 33 other tumours using combined 111In-octreotide and 99mTc-DTPA brain scintigraphy. 111In-octreotide scintigraphy was used to image somatostatin receptors (SSR) and 99mTc-DTPA scintigraphy was used to assess the integrity of the blood-brain barrier (BBB). A total of 32 tumours (65%) were detected. All SSR positive tumours also had positive 99mTc-DTPA scans and all SSR negative tumours were negative on 99mTc-DTPA scans. Among the tumours located outside the BBB, all meningiomas and two out of six schwannomas were positive on combined SSR/99mTc-DTPA scintigraphy. Among the tumours located inside the BBB, seven out of nine gliomas grade I-III were negative, whereas all glioblastomas were positive. Other positive tumours included one malignant non-Hodgkin lymphoma and two cerebral metastases. SSR scintigraphy alone was non-specific in the diagnosis of meningiomas, as 16 non-meningiomatous tumours also had positive SSR scans probably due to a breakdown of the BBB (excluding the malignant lymphoma). Measuring the tumour-to-background ratio on SSR scans improved specificity, but sensitivity was decreased below 70% because some meningiomas were only slightly positive. Only the ratio of SSR scintigraphy to conventional 99mTc-DTPA brain scintigraphy (SSR-to-BS index) allowed a reliable differentiation of meningiomas from other CNS tumours, most notable from schwannomas (sensitivity: 94%; specificity: 100%). Our results support the usefulness of combined SSR and conventional brain scintigraphy in the noninvasive pre-operative diagnosis of meningiomas.
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PMID:Noninvasive differentiation of meningiomas from other brain tumours using combined 111Indium-octreotide/99mtechnetium-DTPA brain scintigraphy. 895 37

We present the pharmacokinetical aspects of somatostatin receptor scintigraphy in rats with the radioiodinated [Tyr3]octreotide and 111In-labeled [DTPA-D-Phe1]octreotide. The residence time of both radionuclides in somatostatin receptor-positive tissues and tumors is completely different, indicating the difference in metabolism of the two radiopharmaceuticals. The effects of the injected radioactive dose and mass of the radioligand and its injection rate on the biodistribution is intensively studied. We found in rat that the uptake of radioactivity in somatostatin receptor-positive tissues is a bell-shaped function of the injected mass depending on the tissue under study, being optimal between 0.5-5 micrograms. This indicates that the sensitivity of the detection of somatostatin receptor-positive tumor by receptor scintigraphy may be improved by varying the mass of the radiopharmaceutical, which has also been confirmed in patient studies. Priming with somatostatin analogues at various time points relative to the radioligand was studied as well. In all the somatostatin receptor-positive tissues we found a significant change in % injected dose uptake of radioactivity, depending on the ligand, its mass and the tissue under study. This might also be a means to increase the target to background ratio in somatostatin receptor scintigraphy. The possible role of the radiopharmaceutical [111In-DTPA-D-Phe1]RC-160 in somatostatin scintigraphy in visualizing somatostatin receptor-positive tumors that do not bind octreotide, for instance somatostatin receptor subtype 4, is discussed. Internalization of the receptor-ligand and metabolism of the radioiodinated and 111In-labeled somatostatin analogues were studied in vitro and in vivo to get insight into metabolism of the radioligand. Internalization of the radioligand is of special importance when radiotherapy of certain somatostatin receptor-positive human tumors with alpha- or beta-emitting radiolabeled somatostatin analogues is considered. Further, peptide receptor radionuclide therapy with several radionuclides is reviewed.
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PMID:Studies on radiolabeled somatostatin analogues in rats and in patients. 896

Octreotide (OCT) administration provides a biochemical cure in most acromegalic patients. This drug, however, causes several side effects and is very expensive. Acute testing has been reported to predict chronic responsiveness to OCT administration. The aim of this retrospective study was to evaluate which test, if any, among acute testing, short-term (1 month) administration, and 111In-pentetreotide (111In-DTPA-Phe-D-OCT) scintigraphy, is best in predicting response to long-term OCT treatment. Sixty-eight patients with active acromegaly were studied. An acute test (100 micrograms sc OCT) was performed as usual: a GH decrease greater than or equal to 50% of baseline was considered a positive response. GH and insulin-like growth factor I (IGF-I) were then assayed after 1 month (300 micrograms daily) and 3 months (150-600 micrograms daily) of OCT administration. GH was considered normalized when decreased less than or equal to 5 micrograms/L. Twenty-six of 68 patients were subjected to 111In-pentetreotide scintigraphy. Linear correlation analysis of the results was performed. Sensitivity, specificity, and positive and negative predictive values of the three tests were also calculated. Thirty-eight of 68 patients (56%) responded to the acute test. Among these 38 patients, 20 experienced normalization of GH and IGF-I levels during long-term therapy, as did 8 patients who did not respond to the acute test. No significant correlation was found between GH percent decrease during acute testing and long-term therapy (r = 0.11). Seven patients who responded to the acute test and 2 who did not respond had adenoma shrinkage during therapy. Conversely, GH and IGF-I decrease after short-term treatment significantly correlated with long-term treatment (r = 0.76 and 0.64, P < 0.01). Of the 26 patients subjected to 111In-pentetreotide scintigraphy, 13 had significant tracer uptake: normalization of GH and IGF-I was obtained in 8 patients. A significant correlation was found between tracer uptake and GH/IGF-I inhibition after 3 months of therapy (r = 0.6; P < 0.05). In the whole population, the positive predictive value of acute testing, short-term OCT administration, and 111In-penetreotide scintigraphy was 53%, 70%, and 73%, respectively, when the GH normalization (< 5 micrograms/L) after 3 months of therapy was considered. Moreover, 111-In-pentetreotide scintigraphy had the highest specificity (100% in patients with baseline GH values below 50 micrograms/L) compared with that of acute testing and short-term OCT administration. The acute test cannot be considered as a valuable index to identify patients' responsiveness to long-term OCT therapy, but it can be useful to test tolerability. By contrast, 1 month of OCT administration or the in vivo imaging of somatostatin receptors by 111-In-pentetreotide might better indicate the patients who might effectively benefit from this treatment.
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PMID:Prediction of efficacy of octreotide therapy in patients with acromegaly. 896 77

Scintigraphy with [111In-DTPA-D-Phe]-octreotide is a recently developed technique for imaging somatostatin receptors in many neuroendocrine tumors. A good correlation between high [111In-DTPA-D-Phe]-octreotide uptake and the response to octreotide therapy has been proved in TSH- and GH-secreting pituitary adenomas, while few and conflicting scintigraphic data on somatostatin receptors in non-functioning tumors have been reported in the literature. The present study presents the results obtained with [111In-DTPA-D-Phe]-octreotide scintigraphy in thirteen patients with GH-secreting pituitary adenoma, four patients with inappropriate TSH-secretion and twelve patients with non-functioning pituitary adenoma. Twelve out of the 13 patients with GH-secreting pituitary adenomas had a positive scan; moreover, in 5/6 patients with a GH-secreting microadenoma (tumor size range 5-8 mm) a positive scan was found. Two TSH-secreting macroadenomas had a positive scan while a negative scan was obtained for a TSH-secreting pituitary microadenoma and in a patient with non-neoplastic, inappropriate secretion of TSH. Finally, only 2/12 patients with non-functioning pituitary adenoma showed a positive scan. In conclusion, [111In-DTPA-D-Phe]-octreotide scintigraphy is a useful tool to confirm the presence of somatostatin receptors in selected patients with GH- and TSH-secreting pituitary adenoma. The role of [111In-DTPA-D-Phe]-octreotide scintigraphy in non-functioning pituitary tumors remains to be established, but it could be useful for octreotide treatment in patients who refuse surgery or who are poor surgical candidates.
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PMID:[111In-DTPA-D-Phe]-octreotide scintigraphy in functioning and non-functioning pituitary adenomas. 900 59


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